Clinical trial · Interventional
Study of MLN8237 in Participants With Advanced Solid Tumors
An Open-label, Phase 1 Study of the Relative Bioavailability, Food Effect, Safety and Tolerability of MLN8237 in Patients With Advanced Solid Tumors
NCT00962091CI-TRIAL-00037555completedPhase 1Results postedClinicalTrials.gov clinicaltrialsProvenance
- Source
- ClinicalTrials.gov
- Retrieved
- Sep 8, 2026
- Layer
- normalized (units and labels harmonized; values unchanged)
- Run
- ING-CLINICALTRIALS-20260908-000001
Summary
Brief summary (as posted)
The purposes of this study were to estimate the relative (Rel) bioavailability (BA) of an oral solution (OS) formulation of alisertib in reference to a powder-in-capsule (PIC) formulation, to characterize the effect of food on the single-dose pharmacokinetics (PK) of alisertib OS and enteric-coated tablets (ECT), to characterize the multiple-dose safety, tolerability, and steady-state PK of alisertib administered as an OS, and to characterize the multiple-dose safety and tolerability of alisertib administered as an ECT.
Conditions
Conditions (1)
Free-text conditions as registered, with the CancerIndex entity they were reconciled to and the match type.
| Condition (as posted) | Mapped entity | Match | Confidence |
|---|---|---|---|
| Advanced Solid Tumors | Solid Neoplasm | CURATED_BROADER | 0.80 |
Interventions
Interventions (1)
| Intervention | Type | Mapped drug | Match |
|---|---|---|---|
| Alisertib | Drug | Alisertib | ALIAS |
Design
Arms and outcomes
Arms (7)
- type
- EXPERIMENTAL
- label
- Dose Escalation
- description
- A single dose of alisertib 15 mg, oral solution (OS) was administered on Day 1, followed by alisertib 40 mg, powder-in-capsule (PIC), orally, twice a day (BID) on Days 3 through 9, followed by a 14-day rest period in Cycle 1 in a 23-day cycle. A single dose of alisertib 50 mg PIC, orally, was administered on Cycle 2 Day 1 followed by alisertib 40 mg on Days 3 through 9, followed by a 14-day rest period in Cycle 2 in a 23-day cycle. Subsequent cycles, alisertib 40 or 50 mg (individual dosage based on tolerability in Cycles 1 and 2), PIC, orally, BID on Days 1 through 7, followed by a 14-day rest period in 21-day cycles until disease progression, occurrence of an unacceptable alisertib-related toxicity, or the start of another anticancer therapy.
- interventionNames
- Drug: Alisertib
- type
- EXPERIMENTAL
- label
- Part A: Relative Bioavailability OS/PIC (Sequence A)
- description
- A single dose of alisertib 25 mg, OS, administered on Day 1, followed by alisertib 40 mg PIC, orally, BID on Days 3 through 9, followed by a 14-day rest period in Cycle 1, in a 23-day cycle. A single dose of alisertib 50 mg PIC, orally, administered on Cycle 2 Day 1, followed by alisertib 40 mg, PIC, orally, BID on Days 3 through 9, followed by a 14-day rest period in a 23-day cycle. Subsequent cycles, alisertib 40-50 mg (individual dosage based on tolerability in Cycles 1 and 2), PIC, orally, BID on Days 1 through 7, followed by a 14-day rest period in 21-day cycles until disease progression, occurrence of an unacceptable alisertib-related toxicity, or the start of another anticancer therapy.
Eligibility
Eligibility (as posted)
- Sex
- All
- Minimum age
- 18 Years
Show eligibility criteria text
Inclusion Criteria: Each participant must meet all of the following inclusion criteria to be enrolled in the study: * 18 years or older * Histologically or cytologically confirmed metastatic and/or advanced solid tumor * Eastern Cooperative Oncology Group (ECOG) performance status 0 or 1 * Female participants who are post menopausal, surgically sterile, or agree to practice 2 effective methods of contraception or abstain from heterosexual intercourse * Male participants who agree to practice effective barrier contraception or agree to abstain from heterosexual intercourse * Voluntary written consent * Suitable venous access for study-required blood sampling * Measurable disease * Recovered from effects of prior antineoplastic therapy * Meet required entry laboratory and organ function levels Exclusion Criteria: Participants meeting any of the following exclusion criteria are not to be enrolled in the study: * Female participants who are pregnant or lactating * Serious medical or psychiatric illness that could interfere with protocol completion * Major surgery within 14 days of first dose of alisertib * Antineoplastic therapy, radiation therapy or any experimental therapy 21 days prior to first dose of alisertib * Nitrosoureas or mitomycin-C within 6 weeks before the first dose of alisertib. * Autologous stem cell transplant within 3 months before the first dose of alisertib, or prior allogeneic stem cell transplant at any time. * Active infection requiring systemic therapy, or other serious infection * Inability to swallow oral medication * Gastrointestinal (GI) disease or GI procedure that could interfere with oral absorption or tolerance of alisertib * Symptomatic brain metastasis * Uncontrolled cardiovascular condition * Diagnosis or treatment of another malignancy within 2 years preceding first dose of study drug except nonmelanoma skin cancer or in situ malignancy completely resected * Known history of human immunodeficiency virus (HIV) infection, hepatitis B, or hepatitis C * Lactose-intolerant (Parts A and B only) * Prior history of metabolic acidosis (Parts A and B only) * Use of enzyme-inducing antiepileptic drugs such as phenytoin, carbamazepine or phenobarbital, or rifampin, rifabutin, rifapentine or St. John's wort within 14 days prior to the first dose of alisertib * A medical condition requiring use of pancreatic enzymes; or daily, chronic , or regular use of proton pump inhibitors (PPI); or histamine (H2) receptor antagonists. Participants who intermittently use these medications must meet the following: * No use of PPI within 7 days of first dose of alisertib * No use of H2 antagonist or pancreatic enzymes within 24 hours of first dose of alisertib * Participants requiring full systemic anticoagulation
References
Publications (2)
- DERIVEDFalchook GS, Zhou X, Venkatakrishnan K, Kurzrock R, Mahalingam D, Goldman JW, Jung J, Ullmann CD, Milch C, Rosen LS, Sarantopoulos J. Effect of Food on the Pharmacokinetics of the Investigational Aurora A Kinase Inhibitor Alisertib (MLN8237) in Patients with Advanced Solid Tumors. Drugs R D. 2016 Mar;16(1):45-52. doi: 10.1007/s40268-015-0114-8. PMID 26689566
- DERIVEDFalchook GS, Venkatakrishnan K, Sarantopoulos J, Kurzrock R, Mita AC, Fu S, Mita MM, Zhou X, Jung JA, Ullmann CD, Milch C, Rosen LS. Relative bioavailability of a prototype oral solution of the Aurora A kinase inhibitor alisertib (MLN8237) in patients with advanced solid tumors. Int J Clin Pharmacol Ther. 2015 Jul;53(7):563-72. doi: 10.5414/CP202359. PMID 26073352